TAK-683 acetate is a potent fullKISS1 receptor (KISS1R)agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R withEC₅₀values of 0.96 nM and 1.6 nM for human and rat, respectively^[1]. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasmaFSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostatecancer^[1][2][4].

TAK-683 acetate exhibits an IC₅₀value (95% CI) from receptor binding assays is 150-180 pM and EC₅₀value (95% CI) from Ca⁺mobilization assays is 180 (159–203) pM in rat KISS1R-expressing Chinese hamster ovary (CHO) cells^[4].

TAK-683 acetate (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced^[3].
TAK-683 acetate (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer^[3].
TAK-683 acetate (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14^[4].

1358.50

Solid

C₆₆H₈₇N₁₇O₁₅

N-Acetyl-YWNTF{aza}L{Met-R}W-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

H₂O : 5 mg/mL(3.68 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。